| Identification | Back Directory | [Name]
(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE | [CAS]
204067-01-6 | [Synonyms]
PD 176252
(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE
(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
(S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide
1H-Indole-3-propanamide, N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-, (αS)- | [Molecular Formula]
C32H36N6O5 | [MDL Number]
MFCD09971099 | [MOL File]
204067-01-6.mol | [Molecular Weight]
584.67 |
| Chemical Properties | Back Directory | [Boiling point ]
838.8±65.0 °C(Predicted) | [density ]
1.297±0.06 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Powder | [pka]
11.60±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. | [Biological Activity]
Non-peptide gastrin-releasing peptide receptor (GRP-R, BB 2 ) and neuromedin B receptor (NMB-R, BB 1 ) antagonist (K i values are 0.17 and 1.0 nM for BB 1 and BB 2 respectively). Inhibits proliferation of rat C6 glioma cells (IC 50 = 2 μ M) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC 50 = 5 μ M). | [in vivo]
PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice[3]. | [storage]
Store at -20°C | [References]
[1] Ashwood V, et al. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94. DOI:10.1016/s0960-894x(98)00462-4
[2] Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90. DOI:10.1124/mol.110.068288
[3] Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9. DOI:10.1016/s0014-2999(03)01996-4 |
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